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MOHD III > Chemotherapy drugs > Flashcards

Chemotherapy drugs Flashcards

1
Q

alkylating agents

A

form covalent adducts with DNA bases resulting in tumor cell death

    • bischloroethyl amines (nitrogen mustards)
    • nitrosoureas
    • Mechlorethamine
  • can be bifunctional or monofunctional
  • can mutagenic (secondary cancers can result from chemotherapy)
  • myelosuppression and oral/GI mucositis = dose limiting
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2
Q

nitrosourea

A
  • alkylating agent
  • little cross over with other alkylating agents so can use if resistance to other drugs is formed
  • crosses blood brain barrier
  • useful against brain tumors
  • has chloroethyl group
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3
Q

Methotrexate

A
  • inhibitor of human dihydrofolate reductase (DHFR)
  • depletes cells of tetrahydrofolate which is needed for thymine synthesis
  • accumulates in cells as a polyglutamate derivative
  • folic acid analog
  • S phase specific
  • myelosuppressive effects can be ameliorated by combination with Leucovorin
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4
Q

5-fluorouracil

A
  • pyrimidine antagonist
  • S phase specific
  • administered by IV (variable absorption po)
  • direct inhibition of thymidylate synthetase
  • works synergistically with leucovorin for colon cancer treatment
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5
Q

anti-tumor antimetabolites

A
  • agents that inhibit metabolic processes essential in the S phase of the cell cycle
  • methotrexate and purine/pyrimidine antagonists
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6
Q

DNA intercalating agents

A
  • bind to DNA and interfere with DNA replication causing mutations
  • anthracyclines (doxorubicin and daunorubicin)
  • interfere with DNA topoisomerase II function
  • cardiac toxicity = dose limiting factor
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7
Q

bleomycin

A
  • cytotoxic action: DNA strand scission
  • generates free radicals
  • pulmonary fibrosis = side effect
  • good in ABVD Hodgkin lymphoma combo treatment therapy
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8
Q

Mitotic spindle poisons

A
  • M phase specific agents interfere with mitotic spindle function during mitosis
  • bind to tubulin protein subunits of microtubule with polymerization or depolymerization
  • Vinca alkaloids (vincristine/ vinblastine)
  • Taxanes (paclitaxel)
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9
Q

vincristine

A
  • mitotic spindle poison
  • non-dose limiting bone marrow depression
  • dose limitied neurotoxicity
  • MOPP regime hodgkins-lymphoma
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10
Q

Vinblastine

A
  • mitotic spindle poison

- bone marrow depression = dose limiting

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11
Q

Topoisomerase inhibitors

A
  • elicit DNA damage via interaction with DNA topoisomerase/DNA complexes
  • interfere with the religation of single or double stranded DNA stranded breaks
  • DNA topoisomerase I: topotecan and irinotecan
  • DNA topoisomerase II: etoposide, daunorubicin, and doxorubicin
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12
Q

cisplatin and carboplatin

A
  • platinum cooridation complex
  • forms adducts with DNA bases and exert toxicity in similar mechanism of classical alkylating agents
  • causes nephrotoxicity (reversible with hydration)
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13
Q

aromatase inhibitors

A
  • block estrogen synthesis through aromatase enzyme

- Ietrozole, anastrozole, exemestane

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14
Q

Leuprolide

A
  • synthetic gonadotropin-releasing hormone (GnRH) receptor agonist
  • prostate cancer treatment
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15
Q

flutamide

A
  • prostate cancer treatment
  • ineffective against prostate cancer alone
  • used in combo with leuprolide
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16
Q

Enzalutamide

A

alternative hormonal therapies for treatment of castration-resistant prostate cancers
-androgen receptor antagonists used in conjunction with GnRH agonists

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17
Q

prednisone

A
  • adrenocorticosteroid
  • multidrug regimen used for leukemia, lymphoma, and myeloma
  • anti-proliferative and lymphocytic effects on immune cells
  • used as palliative agents in other cancers to reduce inflammation and nausea
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18
Q

Erlotinib

A
  • epidermal growth factor (EGF) receptor protein tyrosine kinase inhibitor
  • mutationally activated
  • NSCLC (non-small cell lung cancer)
  • head and neck cancers
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19
Q

Lapatinib

A
  • HER2 receptor protein tyrosine kinase inhibitor
  • overexpressed by gene amplification
  • breast cancer
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20
Q

Imatinib

A
  • Abl protein tyrosine kinase inhibitor

- activated by rearrangement/fusion of Bcr and Abl protein tyrosine kinase genes in chronic myelogenous leukemia

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21
Q

Venmurafenib

A
  • B-raf protein kinase inhibitor

- mutationally activated in melanomas

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22
Q

Cetuximab

A
  • EGF receptor protein tyrosine kinase inhibitor
  • chimeric EGFR antibody
  • colon cancer
  • head and neck cancer
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23
Q

Trastuzumab

A
  • HER2 receptor protein tyrosine kinase inhibitor
  • humanized HER2 antibody
  • Treat breast cancer
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24
Q

Rituximab

A
  • monoclonal antibody directed against CD20 surface antigen on B cells
  • expressed on non hogkin lymphoma
  • chronic lymphocytic leukemia
  • chimeric IgG
  • Adverse: association with PML (progressive multifocal leukoencephalopathy)
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25
Q

Brentuximab Vedotin

A
  • CD30 surface antigen
  • expressed on some hodgkin and non-hodgkin lymphoma cells
  • chimeric IgG conjugated to mitotic spindle poison vedotin
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26
Q

BCG - TheraCys

A
  • adjuvant immune system (immunostimulant)
  • live attenuated bacillus calmette-guerin
  • increase APC (antigen presenting cell) activity
  • Bladder cancer treatment
  • direct activation of leukocytes (macrophages) can result in systemic inflammation and septic shock
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27
Q

Aldesleukin, Proleukin (IL-2)

A

IL-2 cytokine (immunostimulant)

  • increased proliferation of activated T cells, production of IFN-gamma, and cytotoxic killer cell activity
  • side effects arise as it amplifies all immune responses in host
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28
Q

Actimmune (IFN-gamma)

A

IFN-gamma (immunostimulant)

- treats severe recurrent infections

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29
Q

Betaseron, Extavia, Avonex, Rebif (IFN-beta)

A

IFN- beta (immunostimulant)

  • multiple sclerosis
  • reduction of pro-inflammatory cytokines
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30
Q

Ipilimumab

A

immune checkpoint inhibitor

  • fully human antibody to CTLA-4
  • activates naive T cell in lymph node
  • can cause severe and fatal immune mediated rxns cased by t cell activation and prolifereation esp in GI tract
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31
Q

Nivolumab

A

immune checkpoint inhibitor

  • fully human antibody to PD-1
  • effector T cell function in the periphery
  • synergistic effects on tumor regression with ipilimumbab in metastatic melanoma, colorectal, and renal cell cancer
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32
Q

Cyclophosphamide - (cytoxan)

A

immunosuppression by cross-linking DNA and killing proliferating cells:
AKA an alkylating agent
- causes hemorrhagic cystitis which is reversible with Mesna

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33
Q

Azathioprine - Imuran

A
  • metabolized to 6-mercatopurine
  • further metabolized to: 6-thioguanine
  • metabolized product inhibit purine synthesis
  • inactivated by xanthine oxidase which is:
  • **DECREASED when combined with ALLOPURINOL
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34
Q

Mycophenolate Mofetil (Cell-Cept)

A

hydrolyzed to mycophenolic acid (active form)

-prevents purine synthesis

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35
Q

Methotrexate

A
  • inhibits dihydrofolate reductase (DHFR)
  • prevent synthesis of thymidine and purine nucleotides
  • treatment for Rheumatoid arthritis
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36
Q

Leflunomide - Arava

A

decreased pyrimidine synthesis

- similar to methotrexate

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37
Q

Prednisone

A

Glucocorticosteroid

  • immunosuppressive and anti-inflammatory
  • ligands for glucocorticoid receptors affecting gene transcription
  • immunosuppressive effect: inhibition of cytokine gene expression from antigen activated T cells (thus reduced B cell antibody production as well)
  • first line for solid organ and hematopoietic stem cell transplantation
  • Side effects:
    • Adrenal suppression (suppresses endogenous production of glucocorticosteroids)
    • GI ulceration
    • no serious marrow toxicity

reduced expression of inflammatory cytokines

  • reduced expression of chemokines
  • increased expression of annexins inhibits PLA2 activity and reduces Arachidonic Acid production
  • reduced expression of COX2 leads to reduced prostanoid production
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38
Q

Calcineurin inhibitors

A

cytokine gene expression in antigen activated T cells results from calcineurin dependent dephophorylation of the transcription factor NF-AT
- calcineurin is inhibited by complex formed between endogenous proteins: immunophilins and immuno-suppressive drugs

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39
Q

Cyclosporine (sandimmune)

A
  • used in kidney, liver, & cardiac transplants
  • calcineurin inhibitor
  • adverse effect: Nephrotoxicity (bc NF-AT works in kidney)
  • increased cancer indcidence documented
40
Q

Tacrolimus (Prograf, FK506)

A
  • calcineurin inhibitor

- same as cyclosporine

41
Q

Mammalian target of rapamycin (mTOR) inhibitors

A

serine/threonine kinase important for regulating translation of proteins required for cell proliferation
- inhibited by complex bw endogenous immunophilin, FKBP12, and sirolimus

42
Q

Sirolimus (Rapamune, Rapamycin)

A
  • mTOR inhibitor
  • can be used alone or in combo to preserve solid organ transplants
  • antagonizes tacrolimus effects (bc competitor for same receptor FKBP12
  • synergizes with cyclosporine
  • myelosuppression (bc bone marrow proliferation uses same pathway)
43
Q

Rho(D) immune globulin

A

antibody used to suppress unwanted immune response

  • Rh negative mothers can be sensitized to the foreign D antigen of the Rh-positive fetus
  • mechanism of immune suppression by Rh(D) antibodies is mediated through opsonization and clearance of fetal Rh+ cells before an effective immune response can develop
44
Q

Belatacept (Nulojix)

A

blocks co-stimulatory receptors for immunosuppression
- prevents interaction between B7 (on APC) and CD28 (on T cell)
- no proliferation
- no cytokine production
Adverse effects:
- posttransplant lymphoproliferative disorder (PTLD)
- contraindicated in EBV-negative patients (as they are more susceptible to PTLD)

45
Q

Natalizumab (Tysabri)

A

blocks adhesion molecules for immunosuppression
- blocks interaction between VLA-4 and VCAM-1 (preventing lymphocytes migration from vasculature into inflamed tissue sites)
- used for: relapsing forms of MS and Crohn disease
Adverse effects:
– increased risk of PML

46
Q

Antibodies as immune depleting agents

A
  • produce prolonged (up to one year) depletion of circulating lymphocytes
  • immuno-suppressive at the time of organ transplantation (induction therapy)
47
Q

Anti-T Cell globulin (ATG)

A
  • product of repeated injection of human T cells into horse, rabbit, sheep, or goats
  • blocks T cell surface receptors & opsonizes T cells
  • prolonged T cell depletion
    Adverse effects:
    – cytokine release syndrome
48
Q

Alemtuzumab (campath)

A 
humanized anti-CD52 antibody
- depletes a broad variety of cells involved in immune system
Adverse effects:
-- myelosuppression
-- flu-like symptoms
49
Q

Basiliximab (simulect)

A

Humanized anti-IL 2 receptor (anti-CD25) antibody

  • blocks and opsonizes the alpha chain of IL-2 receptor (CD25) that is present on activated T cells
  • depletes only antigen activated T cells
50
Q

Ocrelizumab

A
  • *first and only approved theray for progressive forms of MS
  • mostly human monoclonal antibody to CD20, a B cell surface antigen
  • opsonizes B cells & reduces circulating numbers of B cells resulting in reduced antibody production
51
Q

Ustekinumab

A

cytokine inhibitor

  • human monoclonal antibody which binds to and interferes with IL-12 & IL-23
  • interferes with development of Th1 and Th17 responses
  • treats: Psoriasis and Crohn’s disease
52
Q

Ixekizumab

A

cytokine inhibitor

  • humanized monoclonal antibody which binds to IL-17 and inhibits its interaction with its receptor
  • inhibits release of proinflammatory cytokines associated with Th17 response
53
Q

DMARDs (disease modifying antirheumatic drugs)

A

reduce communication of cytokines that promote inflammatory process

54
Q

Infliximab (Remicade)

A

Anti-TNFalpha agent
- humanized antibody to TNFalpha
- binds to TNFalpha prevents interaction with its receptor; reduces circulation/localized levels of TNF alpha
Treatment: rheumatoid arthritis and Crohn’s disease
- increased frequency of serious infections (respiratory/urinary)

55
Q

Adalimumbab

A

human antibody to TNF alpha

- similar infliximab

56
Q

Etanercept

A

Fusion protein containing the ligand binding domain the TNFalpha receptor and the Fc domain of human IgG
- similar to infliximab

57
Q

Anakinra

A

anti-IL1 agents

  • competitive IL-1 receptor antagonist (IL-1Ra analog)
  • short half life, daily injection required
58
Q

Jak inhibitor

A

Jak kinases are required mediators of signaling pathways activated by many cytokines

59
Q

Tofacitinib

A

general Jak kinase inhibitor
- oral administration
- inhibits all activity of cytokines required for adaptive immunity
-comparable to anti-TNFalpha agents in rheumatoid arthritis
Adverse effets:
– anemia, neutropenia, general myelosuppression

60
Q

Diphenhydramine (benadryl)

A

antihistamine - first generation

61
Q

Dimenhydrinate (dramamine)

A

first generation anti-histamine

62
Q

cyclizine (Marezine)

A

first generation anti-histamine

63
Q

Promethazine

A

first generation anti-histaine

64
Q

Loratadine (claritin)

A

second generation antihistamine

  • highly selective for H1 sites with few anti-cholinergic side effets
  • penetrate poorly into CNS reducing sedative effects
65
Q

Cetirizine (zyrtec)

A

second generation antihistamine

  • highly selective for H1 sites with few anti-cholinergic side effets
  • penetrate poorly into CNS reducing sedative effects
66
Q

Fexofenadine (Allegra)

A

second generation antihistamine

  • highly selective for H1 sites with few anti-cholinergic side effets
  • penetrate poorly into CNS reducing sedative effects
67
Q

Aspirin

A
  • NSAID
  • ASA (acetylsalicylic acid) rapidly converted to salicylic acid in circulation
  • ASA acetylates and irreversibly inhibits COX1 and COX2
  • salicylic acid a reversible inhibitor or COX1 and COX2
  • *all NSAIDs besides ASA are reversible inhibitors**
  • *only NSAID shown to reduce risk of adverse CV events** (mechanism: loss of cox2 dependant production of PGI2 which antagonizes platelet and vascular effects of TXA2 produced by COX1 dependent activities in platelets
68
Q

Acetaminophen

A

reduced in the presence of peroxides that are elevated at sites of inflammation

  • lacks signigicant effects on platelets, CV, & gastrointestinal systems
  • analgesic and antipyretic effects equivalent to aspirin
69
Q

Celecoxib (celebrex)

A

COX-2 selective NSAIDs

  • GI side effects
  • increased incidence of CV events: hypertension, heart attack, stroke (with long term continuous use)
70
Q

Zileuton

A

leukotriene synthesis inhibitor

- inhibition of 5-lipoxygenase inhibits synthesis of LTB4 and LTD4 in mast cells and eosinophils

71
Q

LTD4

A

leukotriene product

  • increase capillary permeability, promoting localized edema
  • constrictor of bronchial smooth muscle (resulting in difficulty breathing)
  • produced by mast cells
  • attracts eosinophils (leukocytes) to airway leading to increased airway reactivity
72
Q

LTB4

A

leukotriene product

- attracts neutrophils (leukocytes) to airway leading to increased airway reactivity

73
Q

Zafirlukast and Montelukast

A

leukotriene receptor antagonist

  • long term therapy for asthma
  • LTD4 receptor antagonists reduced bronchoconstriction and edema associated with inflammatory responses
74
Q

Anastrozole

A

aromatase inhibitor

- more effective than SERMs in treatment of ER+ breast cancer in postmenopausal women

75
Q

Capecitabine

A

prodrug of 5-FU

  • preferential activation in tumor cells
  • activated by thymidine phosphorylase
76
Q

Doxorubicin and Daunorubicin

A

Anthracycline which are DNA intercalating agents that bind to DNA and interfere with DNA replication cause DNA mutation
- anthracyclines also interfere with DNA topoisomerase II function

77
Q

Diclofenac

A

nonselective cox inhibitor

78
Q

Dimenhydrinate, diphenhydramine, cyclizine, promethazine

A

H1 receptor antagonists
- act as inverse agonists: prevent histamine activation of recpetor as well as reducing basal activity of receptor
- treats: allergic rhinitis, uticaria, motion sickness
Adverse:
– sedation
– non-H1 effects (anticholinergic effects, adrenoreceptor blockade, serotonin receptor blockade, local anesthesia)

79
Q

Dimercaprol

A

used in Chelation therapy

80
Q

EDTA

A

used in Chelation therapy

81
Q

etoposide

A

interferes with DNA topoisomerase II

- substrate transported by the MDR1 drug transporter leading to multidrug resistance

82
Q

exemestane

A

aromatase inhibitors

- more effective than SERMs in treatment of ER+ breast cancers in postmenopausal women

83
Q

indomethacin

A

nonselective COX inhibitor

84
Q

Topotecan and irinotecan

A

interferes with DNA topoisomerase I

- interferes with the religation of the single or double stranded DNA breaks

85
Q

Ketorolac

A

non-selective COX inhibitor

86
Q

Letrozole

A

antagonist of hormone action

87
Q

Leucovorin

A

anti-tumor metabolite
- “folinic acid rescue”: amelioration of myelosuppressive effects of methotrexate when given in the interval between successibe methotrexate treatments

88
Q

Misoprostol

A
  • PGE1 analog

- protects against COX1 inhibition

89
Q

oxytocin

A

-used to induce uterine contractions

90
Q

Paclitaxel

A

mitotic spindle poison

  • block microtubule disassembly
  • ovarian cancer
91
Q

Procarbazine

A

monofunctional alkylating agent

- mutagenic

92
Q

Raloxifene

A
  • antagonists of hormone action

- SERM used for ER+ breast cancer

93
Q

Tamoxifen

A
  • antagonists of hormone action

- SERM used for ER+ breast cancer

94
Q

EDTA

A
  • chelates Ca2+ and Mg2+
  • treats lead poisoning
  • administered as CaNa2EDTA to minimize chelation of Ca2+
95
Q

Succimer

A
  • orally effective chelator
  • treatment for lead poisoning
  • approved for children with lead levels of >45ug/dL
96
Q

Penicillamine

A 
chelator of choice for Wilson's disease 
- being replaced by better tolerated trientine
Adverse effects:
-- cutaneous reactions 
-- Lupus like effects 
-- renal toxicity

MOHD III (5 decks)

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